Design, Synthesis and Biological Evaluation of Novel 3-Oxo-4-Oxa-5α-Androst-17β-Amide Derivatives as Dual 5α-Reductase Inhibitors and Androgen Receptor Antagonists

    May 2017 in “ Bioorganic & medicinal chemistry letters ”
    Kejing Lao, Jie Sun, Chong Wang, Ying Wang, You Qin, Hong Xiao, Hua Xiang
    TLDR New compounds were made that are promising for prostate cancer therapy.
    In a study from 2017, researchers designed and synthesized a series of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives to serve as dual 5α-reductase inhibitors and androgen receptor (AR) antagonists, potentially beneficial for prostate cancer treatment. These compounds showed good inhibitory activities against 5α-reductase and strong binding affinities to the AR, as well as potent anti-proliferative effects on prostate cancer cell lines, particularly the androgen-dependent LNCaP cells. Compounds 11d and 11k emerged as the most effective, with 11k demonstrating a longer plasma half-life of 4 hours and better bioavailability compared to finasteride, a known 5α-reductase inhibitor. Molecular modeling indicated that 11k could bind to the AR similarly to dihydrotestosterone. These findings suggest that compounds 11d and 11k could be promising candidates for prostate cancer therapy.
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